cyclosporine ophthalmic (Rx)

>10%

Pain on instillation of drops (22%)

Ocular burning (17%)

1-10%

Conjunctival hyperemia (6%)

Frequency Not Defined

Conjunctival hyperemia

Discharge

Epiphora

Eye pain

Foreign body sensation

Pruritus

Postmarketing Reports

Hypersensitivity (including eye swelling, urticaria, rare cases of severe angioedema, face swelling, tongue swelling, pharyngeal edema and dyspnea)

Superficial injury of the eye (from the vial tip touching the eye during administration)

Contraindications

Known or suspected hypersensitivity to any of the ingredients in the formulation

Cautions

Remove contact lenses prior to administration

Do not touch eyelids with vial tip to avoid contamination

Do not use with contact lenses; lenses may be reinserted 15 minutes following administration ophthalmic emulsion/solution

Pregnancy

Clinical administration of cyclosporine ophthalmic emulsion 0.05% is not detected systemically following topical ocular administration, and maternal use is not expected to result in fetal exposure to the drug

Oral administration of cyclosporine to pregnant rats or rabbits did not produce teratogenicity at clinically relevant doses

Lactation

Cyclosporine is known to appear in human milk following systemic administration, but presence in human milk following topical treatment has not been investigated; although blood concentrations are undetectable following topical administration of cyclosporine ophthalmic, caution should be exercised when cyclosporine ophthalmic multidose is administered to a nursing woman; the developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for cyclosporine ophthalmic multidose and potential adverse effects on the breast-fed child from cyclosporine

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Mechanism of Action

Exact mechanism of action is not known

Calcineurin inhibitor; immunosuppressive agent when administered systemically

In patients whose tear production is presumed to be suppressed due to ocular inflammation associated with dry eyes, cyclosporine emulsion is thought to act as a partial immunomodulator

Absorption

Emulsion: There was no detectable drug accumulation in blood during 12 months of treatment

Solution: Blood concentrations of cyclosporine after twice daily topical ocular administration into each eye of healthy subjects for up to 7 days, and once on Day 8, were either not detectable or were marginally above the lower limit of assay quantitation of 0.1 ng/mL for up to 2 hr after a single dose, and up to 4 hr after multiple doses

Ophthalmic Administration

Single-use solution or emulsion: After opening for administration to one or both eyes use immediately, and discard remaining contents immediately

Do not administer while wearing contact lenses; remove contacts prior to administration; contacts may reinsert 15 minutes following administration

Storage

Emulsion: Store at 15-25°C (59-77°F)

Solution: Store at 20-25°C (68-77°F); store single-use vials in the original foil pouch